Lerociclib dihydrochloride (G1T38) is a potent, selective and orally bioactive CDK4/CDK6 inhibitor with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. G1T38 is a competitive, nanomolar inhibitor of CDK4/6 with highly selectivity for CDK4-cyclin D1 and CDK6-cyclin D3. G1T38 exhibits a low EC50 (<100 in='' rb='' competent='' cell='' lines='' compared='' to=''>3 μM in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models.

纯度：≥98%

CAS：2097938-59-3